C07J43/00

COMPOUND WITH ANTI-SPORE ACTIVITY AND PHARMACEUTICAL COMPOSITION THEREOF

The present disclosure provides a compound represented by formula (I), or a salt or a stereoisomer thereof. The compound is capable of effectively inhibiting germination of Clostridium difficile spores with a significant bacteriostatic activity. The compound has an excellent prospect for use in preparation of a drug for preventing and/or treating a C. difficile-caused infectious disease, recurrence of the C. difficile-caused infectious disease, or a complication of the C. difficile-caused infectious disease.

Aminosteroids for the Treatment of a PTP1B Associated Disease

This application is directed to the use of aminosteroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes.

Combination of estrogens plus antiprogestins with significant partial agonistic effect as an effective treatment of menopausal symptoms and for prevention of the occurrence of breast cancer

Described herein are compositions and methods for hormone replacement therapy that address the shortcomings of the existing methods. Described herein are pharmaceutically effective partial agonistic antiprogestins. The combined application of estrogens (such as estradiol, estriol and conjugated estrogens) and the disclosed partial agonistic antiprogestins can be used in hormone replacement therapy.

NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF

Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v), and wherein L.sup.1, L.sup.2, L.sup.3, X.sup.1, X.sup.2, Y, R.sup.z4, R.sup.z5, R.sup.z6, n, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.14, R.sup.17, R.sup.19, R.sup.20, R.sup.23a, R.sup.23b, and R.sup.24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.

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COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS

Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3 and A are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.

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Abiraterone Acetate Formulation
20170354665 · 2017-12-14 ·

Pharmaceutical compositions, including unit dosage forms, comprising fine particle abiraterone acetate with or without an antioxidant and or a sequesting agent as well as methods for producing and using such compositions are described.

Prodrugs of 17.BETA.-HSD1-inhibitors

The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R1 to R4 are as defined in the claims. The invention further relates to their use as inhibitors of 17β-HSD1 and in treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17β-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof.

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TGR5 MODULATORS AND METHODS OF USE THEREOF

The application relates to compounds of formula A:

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or a salt, solvate, ester, tautomer, amino acide conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.

NEUROACTIVE STEROIDS AND THEIR METHODS OF USE

Provided herein is a compound of Formula (I), or a pharmaceutically acceptable salt thereof, wherein R.sup.2a, R.sup.2b, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6a, R.sup.6b, R.sup.11a, R.sup.11b, R.sup.15a, R.sup.15b, R.sup.16a, R.sup.16b, R.sup.18, R.sup.19, R.sup.20a, R.sup.20b, X, A, Z, q, u, r, s, t, m, and n are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

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3,3 DISUBSTITUTED 19-NOR PREGNANE COMPOUNDS, COMPOSITIONS, AND USES THEREOF

Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I) and (III):

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where R.sup.1, R.sup.2, R.sup.3, R.sup.3′, R.sup.4, R.sup.6a, R.sup.6a, R.sup.11a, and R.sup.11b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, insomnia, anxiety, depression, traumatic brain injury (TBI), stress, and epilepsy.